Bosentan and Cyclosporine Injection: Interaction Details
AI-assisted, pharmacist-reviewed · Source data updated Aug 8, 2026 · Sources: FDA labeling, DDInter 2.0, cited literature
Bosentan
No brand names on recordCyclosporine Injection
How we grade severity & evidence
Severity levels
- Contraindicated: These should generally not be used together.
- Major: Potentially serious — often needs a change or close monitoring.
- Moderate: Can be significant — usually manageable with monitoring.
- Minor: Usually limited clinical impact.
Evidence grades
- Established: Well documented — supported by controlled studies or strong clinical data.
- Probable: Good supporting evidence, though not definitively proven.
- Suspected: Some evidence suggests this interaction, but it is not well established.
- Possible: Limited or conflicting evidence; the interaction may occur.
- Theoretical: Predicted from the drugs' pharmacology; not yet confirmed in people.
Ratings come from the documented interaction literature and are reviewed by a pharmacist. They describe the documented risk of the combination, not what will necessarily happen to you — your dose, timing, and health picture all matter.
What happens
Reduced cycloSPORINE exposure and increased bosentan exposure
Interaction Deep Dive
Coadministration of bosentan and cycloSPORINE is contraindicated. Coadministration of cycloSPORINE and bosentan resulted in markedly increased plasma concentrations of bosentan. Trough concentrations of bosentan were increased by approximately 30-fold during the first day of concomitant administration with cycloSPORINE3. Also, concomitant use of cycloSPORINE and bosentan may result in decreased cycloSPORINE plasma concentrations. If concurrent therapy is required, monitor circulating cycloSPORINE levels and make appropriate dosage adjustments as necessary 12.
Why it happens (mechanism)
Induction of CYP3A4-mediated metabolism of cycloSPORINE; inhibition of CYP3A4-mediated metabolism of bosentan
Literature reports
3 reports — tap to read
a) In an drug interaction study, trough concentrations of bosentan were increased by approximately 30-fold during the first day of concomitant administration with cycloSPORINE 3.
b) Coadministration of bosentan (250 to 1000 mg every 12 hours based on tolerability) and cycloSPORINE (300 mg every 12 hours for 2 days then dosing to achieve a Cmin of 200 to 250 ng/mL) for 7 days in healthy subjects resulted in decreases in the cycloSPORINE mean dose-normalized AUC, Cmax, and trough concentration of approximately 50%, 30%, and 60% respectively, compared to when cycloSPORINE was given alone 12.
c) In healthy subjects, coadministration of bosentan and cycloSPORINE resulted in time-dependent mean increases in dose-normalized bosentan trough concentrations [ie,, approximately 21-fold on Day 1 and 2-fold on Day 8 (steady state)] compared to when bosentan was given alone as a single dose on Day 1 12.
Common questions
Can I take Bosentan and Cyclosporine Injection together?
Reduced cycloSPORINE exposure and increased bosentan exposure Always confirm with your pharmacist or prescriber before making any change.
How serious is the Bosentan and Cyclosporine Injection interaction?
It is rated contraindicated. These should generally not be used together.
How quickly could this interaction happen?
The documented onset is "rapid". Effects can appear quickly, often within about 24 hours of combining the drugs.
How strong is the evidence for this interaction?
The evidence is graded "probable". Good supporting evidence, though not definitively proven.
Questions for your pharmacist
- Does my dose of Bosentan or Cyclosporine Injection need adjusting while I take them together?
- What symptoms should prompt me to call you or my prescriber right away?
- Does the timing of my doses matter for this combination?
- Is there a safer alternative to one of these medications for me?
References (3)
- Product Information: NEORAL(R) oral soft gelatin capsules oral solution, cyclosporine modified oral soft gelatin capsules oral solution. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2023. DailyMed
- Product Information: SANDIMMUNE(R) oral capsules, oral solution, intravenous injection, cyclosporine oral capsules, oral solution, intravenous injection. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2023. DailyMed
- Product Information: TRACLEER(R) oral tablets, oral suspension tablets, bosentan oral tablets, oral suspension tablets. Actelion Pharmaceuticals US Inc (per FDA), Titusville, NJ, 2024. DailyMed
Keep reading about Bosentan
Keep reading about Cyclosporine Injection
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